Search results for "PIP"

Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.

2003

Galantamine (Reminyl), an approved treatment for Alzheimer's disease (AD), is a potent allosteric potentiating ligand (APL) of human alpha 3 beta 4, alpha 4 beta 2, and alpha 6 beta 4 nicotinic receptors (nAChRs), and of the chicken/mouse chimeric alpha 7/5-hydroxytryptamine3 receptor, as was shown by whole-cell patch-clamp studies of human embryonic kidney-293 cells stably expressing a single nAChR subtype. Galantamine potentiates agonist responses of the four nAChR subtypes studied in the same window of concentrations (i.e., 0.1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg. At concentrations10 microM, gal…

Pentafulvene durch Aminomethinylierung des Cyclopentadiens

1986

Aus der Dreikomponentenreaktion von Cyclopentadien (1) mit s-Triazin (2) und einem sekundaren Amin 4 gehen die cyclisch N,N-disubstituierten Pentafulven-6-amine 5 und die cyclisch N1,N1-disubstituierten N2-(6-Pentafulvenyl)formamidine 7 hervor. Unter den biologischen Eigenschaften der neuen Verbindungen ist besonders die anthelminthische Wirkung von 5d interessant. Pentafulvenes by Aminomethynylation of Cyclopentadiene The three component reaction comprising the interaction of cyclopentadiene (1) with s-triazine (2) and a secondary amine 4 leads to the cyclic N,N-disubstituted pentafulven-6-amines 5 and the cyclic N1,N1-disubstituted N2-(6-pentafulvenyl)formamidines 7. Among the biological …

Solution processable piperazine and triphenyl moiety containing non-symmetric bis-styryl-DWK type molecular glasses with light-emitting and amplified…

2018

A series of 2,6-bis-styryl-4H-pyran-4-ylidene fragment containing glassy organic compounds with chemically stable bonding of amorphous phase promoting bulky triphenyl moieties through piperazine structural fragment (DWK-T dyes) in a form of 2-(5,5,5-triphenylpentyl)piperazin-1-yl)styryl)-substituent have been synthesized and investigated as the potential gain medium component for organic solid state laser applications. Physical properties of the dyes vary and are mostly depending from the other styryl-substituent attached to the 4H-pyran-4-ylidene backbone fragment in 6-position. Thermal stability of synthesized dyes is above 312°C with the glass transitions from 97°C to 109°C. Obtained nea…

Micromorfologia fogliare comparata ed anatomia generale di Epipactis microphylla (Ehrh.) SW. ed E. helleborine (L.) Crantz (Orchidaceae) in Sicilia

2009

From attraction to repulsion : anion–π interactions between bromide and fluorinated phenyl groups

2011

Anion–π interactions in crystals of fluorobenzyl ammonium salts depend on the degree of fluorination at the aromatics.

Synthesis and conformational analysis of tetrahydroisoquinoline- and piperidine-fused 1,3,4,2-oxadiazaphosphinanes, new ring systems

2006

Abstract Through cyclization of tetrahydroisoquinoline and piperidine 1,2-hydrazino alcohols with phenylphosphonic dichloride and phenyl dichlorophosphate, P-epimeric diastereomers of 1,6,7,11b-tetrahydro-4H-1,3,4,2-oxadiazaphosphino[5,4-a]isoquinoline-3-oxides ( 13 and 14 ), 1,6,11,11a-tetrahydro-4H-1,3,4,2-oxadiazaphosphino[4,5-b]isoquinoline-3-oxides ( 15 and 16 ) and 1,6,7,8,9,9a-hexahydro-4H-pyrido[1,2-d][1,3,4,2]oxadiazaphosphinane-3-oxides ( 17 and 18 ), the first representatives of these ring systems, were prepared. NMR and X-ray diffraction studies revealed that, independently of the P-substituent and the relative configuration of the phosphorus atom, 13 , 14 , 17 and 18 could be c…

Synthesis of Piperidines and Dehydropiperidines

2017

Abstract The present review focuses on strategies for the construction of piperidines and dehydropiperidines, which have appeared in the literature since 2003/2004 through mid-2016. Synthetic methods involving the construction of the six-membered ring from essentially acyclic starting materials in intra- or intermolecular will be highlighted and discussed. In contrast, methods using only the decoration or modification of previously generated pyridines or piperidines will not be part of this review. The published syntheses will be categorized based on the topology of the bond forming events generating the piperidine core.

Biomimetic diels–alder cyclizations for the construction of the brevianamide, paraherquamide, sclerotamide, asperparaline and VM55599 ring systems

1998

Abstract A potentially bio-mimetic Diels–Alder cyclization to construct the bicyclo[2.2.2] ring system common to the paraherquamides, marcfortines, sclerotamides, brevianamides, VM55599, and asperparaline is reported. Epi-deoxybrevianamide E (22) is converted into the corresponding lactim ether (23) and then oxidized with DDQ to provide an azadiene (24) which is tautomerized in the presence of base to azadiene 25 which, spontaneously cyclizes to give a 2:1 mixture of cycloadducts 26 and 27. These cycloadducts are each in turn, converted into d , l -C-19-epi-brevianamide A (20) and d , l -brevianamide B (6). The stereochemical implications of the [4+2] cycloaddition is discussed in the conte…

Anti-Pseudomonas aeruginosa activity of hemlock (Conium maculatum, Apiaceae) essential oil

2018

Conium maculatum is a nitrophilous weed belonging to the Apiaceae family and occurring in hedgerows, pastures, waste ground, along rivers and roadsides. Little is known on the chemistry and bioactivity of other secondary metabolites occurring in the plant. In the present work, we have analysed the chemical composition and antimicrobial activity of the essential oils hydrodistilled from leaves and inflorescenes of C. maculatum growing in Sicily, Italy. The composition of essential oils was achieved by gas chromatography-mass spectrometry (GC-MS) analysis, whereas the inhibitory effects on the growth of two Gram negative strains, namely Escherichia coli and Pseudomonas aeruginosa were assesse…

Bioactive aristolactams from Piper umbellatum.

2007

Four alkaloids named piperumbellactams A-D (1-4) were isolated from branches of Piper umbellatum together with known N-hydroxyaristolam II (5), N-p-coumaroyl tyramine (6), 4-nerolidylcatechol (7), N-trans-feruloyltyramine, E-3-(3,4-dihydroxyphenyl)-N-2-[4-hydroxyphenylethyl]-2-propenamide, beta-amyrin, friedelin, apigenin 8-C-neohesperidoside, acacetin 6-C-beta-d-glucopyranoside, beta-sitosterol, its 3-O-beta-d-glucopyranoside and its 3-O-beta-d-[6'-dodecanoyl]-glucopyranoside. Glycosidase inhibition, antioxidant and antifungal activities of these compounds were evaluated. Compounds 1-3 showed moderate alpha-glucosidase enzyme inhibition with IC50 values 98.07+/-0.44, 43.80+/-0.56 and 29.64…